MX360932B - Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. - Google Patents

Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.

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Publication number
MX360932B
MX360932B MX2016003137A MX2016003137A MX360932B MX 360932 B MX360932 B MX 360932B MX 2016003137 A MX2016003137 A MX 2016003137A MX 2016003137 A MX2016003137 A MX 2016003137A MX 360932 B MX360932 B MX 360932B
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Prior art keywords
braf
inhibitors
conferring resistance
mutations conferring
mutations
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MX2016003137A
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English (en)
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Levi Garraway
Caroline Emery
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Dana Farber Cancer Inst Inc
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Publication of MX360932B publication Critical patent/MX360932B/es

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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
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    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • C12Y207/00Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/11Protein-serine/threonine kinases (2.7.11)
    • C12Y207/11001Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
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Abstract

La presente invención se refiere a un método para identificar un inhibidor de BRAF de segunda generación, que comprende; a) seleccionar un fármaco potencial utilizando un modelado asistido por computadora con una estructura tridimensional de cristal o de la solución de un polipéptido de BRAF mutante, en donde el polipéptido de BRAF mutante comprende una secuencia de aminoácidos que tiene al menos una sustitución de aminoácidos en comparación con un polipéptido de BRAF V600E que tiene una secuencia SEQ ID NO: 4, la al menos una sustitución de aminoácidos confiere resistencia a uno o más inhibidores de BRAF en el polipéptido de BRAF mutante, en donde la al menos una sustitución de aminoácidos se selecciona del grupo que consiste de A29, H72, S113, S124, P162, C194, L227, P231, C251, V291, Q329, K483, L495, T521, V528, D587, P655, S657, S683, P686, C696, L697, P722, F738 y C748; b) poner en contacto el fármaco potencial con el polipéptido de BRAF mutante; y c) detectar la interacción del fármaco potencial con el polipéptido de BRAF mutante; en donde un compuesto que es capaz de interactuar con el polipéptido de BRAF mutante se identifica como un inhibidor de BRAF de segunda generación.
MX2016003137A 2010-02-25 2011-02-22 Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. MX360932B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30827510P 2010-02-25 2010-02-25
PCT/US2011/025645 WO2011106298A1 (en) 2010-02-25 2011-02-22 Braf mutations conferring resistance to braf inhibitors

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MX360932B true MX360932B (es) 2018-11-21

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MX2012009784A MX340392B (es) 2010-02-25 2011-02-22 Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.
MX2016003137A MX360932B (es) 2010-02-25 2011-02-22 Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.

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US (2) US8637246B2 (es)
EP (2) EP3028699B1 (es)
JP (1) JP5933459B2 (es)
KR (1) KR101814223B1 (es)
CN (1) CN103002894B (es)
AU (1) AU2011221227B2 (es)
BR (1) BR112012021411A2 (es)
CA (1) CA2789696C (es)
ES (2) ES2576061T3 (es)
MX (2) MX340392B (es)
RU (1) RU2571930C2 (es)
WO (1) WO2011106298A1 (es)

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WO2015039107A1 (en) 2013-09-16 2015-03-19 The Johns Hopkins University Activities of multiple cancer-related pathways are associated with braf mutation and predict the resistance to braf/mek inhibitors in melanoma cells
CN111534580A (zh) * 2013-12-28 2020-08-14 夸登特健康公司 用于检测遗传变异的方法和***
WO2019195959A1 (en) 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
WO2020145734A1 (ko) * 2019-01-11 2020-07-16 주식회사 진캐스트 Braf 돌연변이 검출을 위한 dna 중합효소 및 이를 포함하는 키트
EP3993875A4 (en) * 2019-07-02 2023-08-02 Effector Therapeutics, Inc. METHODS OF TREATING BRAF MUTATION CANCER CELLS
CN111349704B (zh) * 2020-03-17 2020-11-24 河北医科大学第三医院 肝癌的诊断产品和治疗组合物

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